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Assay Detail

CHEMBL4707265

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of HDAC6 in human MCF7 cells assessed as increase in acetylated alpha-tubulin at Lys40 residue incubated for 3 hrs by ELISA
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type MCF7
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Histone deacetylase 6 (CHEMBL1865)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
Chen D,Soh CK,Goh WH,Wang H
J Med Chem (2018) 61 : 1552 -1575
PubMed 29360358 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 6.58 6.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4749655 1 6.72
CHEMBL4744689 1 6.66
CHEMBL98 VORINOSTAT 4.0 1 6.37
CHEMBL521851 PICTILISIB 2.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4749655 EC50 = 190.0 nM 6.72
CHEMBL4744689 EC50 = 220.0 nM 6.66
CHEMBL98 VORINOSTAT EC50 = 430.0 nM 6.37
CHEMBL521851 PICTILISIB EC50 > 30000.0 nM -